DETAILED ACTION
Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
Election/Restrictions
Applicant's election with traverse of compound of claim 3 (i.e., (1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3- fluoro-4-(4-methoxyphenyl) pyrrolidin-3-yl] carbonyl}-4-(methoxymethyl) pyrrolidin-3-yl]-5- (trifluoromethyl)phenyl} piperidine-4-carboxylic acid)
PNG
media_image1.png
556
664
media_image1.png
Greyscale
along with the elected solar urticaria in the reply filed on 09/02/2025 is acknowledged and maintained.
Priority
This application is a 35 USC § 371 National Stage application of International Application No. PCT/JP2021/022048, filed June 10, 2021, which claims to Japanese. Application Serial No. JP2020-101162, filed June 10, 2020.
Status of Claims
Acknowledgement is made of the receipt and entry of the amendment to the claims filed on January 30, 2026. Claims 1 and 4-7 and new claims 12-27 are pending. Based on the amendment to claim 4 which in turns causes claim 7 to be dependent on claim 4, claim 4 and 7 are withdrawn as being drawn to nonelected species. Claim 16 is withdrawn as being drawn to nonelected species. Therefore, claims 4, 7 and 16 are withdraw. Claims 2-3, 8-11 are canceled. Claims 1, 5-6, 12-15, and 17-27 are examined in accordance to the elected species.
Action Summary
Claims 1-7 rejected on the judicially-created basis that it contains an improper Markush grouping of alternatives, are withdrawn in light of the deletion of preventing.
Claims 1-7 rejected under 35 U.S.C. 103 as being unpatentable over Yamamoto et al (9,981,960 B2) in view of Bouix-Peter (US9,353,083 B2) and McNeil et al (Skin Therapy Letter, Volume 23 Number 6, December 1, 2018), are withdrawn in light of the claim amendment.
Claims 1-7 rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-32 of U.S. Patent No. 9,981,960 B2 in view of Bouix-Peter (US9,353,083 B2) and McNeil et al (Skin Therapy Letter, Volume 23 Number 6, December 1, 2018), are withdrawn in light of the claim amendment.
Claims 1-7 rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-5 of U.S. Patent No. 11,053,217 B2 in view of Yamamoto et al (9,981,960 B2), Bouix-Peter (US9,353,083 B2) in view of McNeil et al (Skin Therapy Letter, Volume 23 Number 6, December 1, 2018), are withdrawn in light of the claim amendment.
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
Claims 1, 5-6, 12-15, and 17-27 are rejected under 35 U.S.C. 103 as being unpatentable over Yamamoto et al (9,981,960 B2) in view of Bouix-Peter (US9,353,083 B2) and McNeil et al (Skin Therapy Letter, Volume 23 Number 6, December 1, 2018).
Yamamoto teaches a method for treating diseases and/or symptoms in which activation of melanocortin 1 receptor (MC1R) is involved, the method comprising administering to a patient in need thereof an effective amount of a pyrrolidine compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the diseases and/or symptoms is rheumatoid arthritis, gouty arthritis, osteoarthrosis, inflammatory bowel disease, systemic sclerosis, psoriasis, fibrosis, protoporphyria, systemic lupus erythematosus, melanoma, skin cancer, vitiligo, hair loss, pain, ischemia/reperfusion damage, cerebral inflammatory disease, hepatitis, septicemia/septic shock, nephritis, transplantation, HIV disease exacerbation, vasculitis, uveitis, retinitis pigmentosa, age-related macular degeneration, celiac disease, nephrotic syndrome, or melanoma invasion. (See claims 1 and 25.) Moreover, Yamamoto teaches the compound of the formula (I) includes 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidin-3-yl] carbonyl}-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl} piperidine-4-carboxylic acid. (See claim 18.) This compound is the same as the claimed elected compound. Yamamoto teaches the compound can be administered to a patient (a human or animal) using an appropriate method of administration in accordance with the dosage form (e.g., intravenously, orally, percutaneously, or topically). (See lines 51-57 of column 64.) Percutaneous is the same as transdermal. Furthermore, Yamamoto teaches the compound can be used preferably in about 0.01 to 500 mg/person/day. (See lines 1-11 of column 65.)
Yamamoto does not teach solar urticaria as the elected photoallergic dermatitis. Moreover, Yamamoto does not teach 50-600 mg/da. However, the amount of 0.01-500 mg/day of Yamamoto substantially overlaps with the claimed amount.
Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease. (See claim 4.)
McNeil afamelanotide is composed of a linear peptide of thirteen amino acids, two of which differ from α-MSH. These two different amino acids increase the affinity of afamelanotide to the melanocortin 1 receptor (MC1R), which in turn increase the stability, potency, and half-life of afamelanotide. Afamelanotide, like α-MSH, binds to MC1R in dermal cells and in melanocytes, thereby stimulating melanocyte production of eumelanin as well as melanocyte proliferation. Eumelanin exhibits numerous roles, including photoprotection against ultraviolet (UV) light and scavenging of free radicals, while also filtering out longer wavelengths of visible light. Therefore, afamelanotide is photoprotective against visible light photosensitivity and, thus, it is an effective treatment option for disorders such as erythropoietic protoporphyria (EPP), solar urticaria, and polymorphic light eruption (PMLE). (See Introduction Section.) Moreover, McNeil teaches afamelanotide, an α-melanocyte stimulating hormone analogue, has become an emerging therapeutic option for a variety of skin conditions previously refractory to other treatments. Its efficacy has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. Its relatively low risk side effect profile makes it an attractive treatment option and also paves the way for innovative use in other disorders. (See Abstract.) McNeil further teaches Solar urticaria is a chronic photosensitivity disorder characterized by an itch, wheal and flare reaction that occurs within minutes of sunlight exposure. (See Solar Urticaria Section.)
It would have been prima facie obvious to one of ordinary skill in the art at the time the invention was filed to modify the method taught by Yamamoto by including a solar urticaria excluding photodermatosis and 50-600 mg/day to give Applicant’s claimed invention. One would have been motivated to do so, because Yamamoto teaches the compound has melanocortin 1 receptor (MC1R) agonistic activity can be administered in the amount of 0.01 to 500 mg/day, where said amount substantially overlap with the amount claimed, because Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease, and also because McNeil teaches other MC1R agonist such afamelanotide has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. One would reasonably expect the method of the compound of Yamamoto to successfully treat solar urticaria excluding protoporphyria.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 1, 5-6, 12-15, and 17-27 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-32 of U.S. Patent No. 9,981,960 B2 in view of Yamamoto et al (9,981,960 B2), Bouix-Peter (US9,353,083 B2) and McNeil et al (Skin Therapy Letter, Volume 23 Number 6, December 1, 2018).
The U.S. patent teaches a method for treating diseases and/or symptoms in which activation of melanocortin 1 receptor (MC1R) is involved, the method comprising administering to a patient an effective amount of a pyrrolidine compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the diseases and/or symptoms is rheumatoid arthritis, gouty arthritis, osteoarthrosis, inflammatory bowel disease, systemic sclerosis, psoriasis, fibrosis, protoporphyria, systemic lupus erythematosus, melanoma, skin cancer, vitiligo, hair loss, pain, ischemia/reperfusion damage, cerebral inflammatory disease, hepatitis, septicemia/septic shock, nephritis, transplantation, HIV disease exacerbation, vasculitis, uveitis, retinitis pigmentosa, age-related macular degeneration, celiac disease, nephrotic syndrome, or melanoma invasion. (See claims 1 and 25.) Moreover, Yamamoto teaches the compound of the formula (I) includes 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidin-3-yl] carbonyl}-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl} piperidine-4-carboxylic acid. (See claim 18.) This compound is the same as the claimed elected compound.
The U.S. patent claims do not teach solar urticaria as the elected photoallergic dermatitis and 50-600 mg/day. Moreover, the U.S. patent claims do not teach topical, transdermal, oral, and intravenous administration along with a human patient.
Yamamoto teaches a method for treating diseases and/or symptoms in which activation of melanocortin 1 receptor (MC1R) is involved, the method comprising administering to a patient in need thereof an effective amount of a pyrrolidine compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the diseases and/or symptoms is rheumatoid arthritis, gouty arthritis, osteoarthrosis, inflammatory bowel disease, systemic sclerosis, psoriasis, fibrosis, protoporphyria, systemic lupus erythematosus, melanoma, skin cancer, vitiligo, hair loss, pain, ischemia/reperfusion damage, cerebral inflammatory disease, hepatitis, septicemia/septic shock, nephritis, transplantation, HIV disease exacerbation, vasculitis, uveitis, retinitis pigmentosa, age-related macular degeneration, celiac disease, nephrotic syndrome, or melanoma invasion. (See claims 1 and 25.) Moreover, Yamamoto teaches the compound of the formula (I) includes 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidin-3-yl] carbonyl}-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl} piperidine-4-carboxylic acid. (See claim 18.) This compound is the same as the claimed elected compound. Yamamoto teaches the compound can be administered to a patient (a human or animal) using an appropriate method of administration in accordance with the dosage form (e.g., intravenously, orally, percutaneously, or topically). (See lines 51-57 of column 64.) Percutaneous is the same as transdermal. Furthermore, Yamamoto teaches the compound can be used preferably in about 0.01 to 500 mg/person/day. (See lines 1-11 of column 65.)
Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease. (See claim 4.)
McNeil afamelanotide is composed of a linear peptide of thirteen amino acids, two of which differ from α-MSH. These two different amino acids increase the affinity of afamelanotide to the melanocortin 1 receptor (MC1R), which in turn increase the stability, potency, and half-life of afamelanotide. Afamelanotide, like α-MSH, binds to MC1R in dermal cells and in melanocytes, thereby stimulating melanocyte production of eumelanin as well as melanocyte proliferation. Eumelanin exhibits numerous roles, including photoprotection against ultraviolet (UV) light and scavenging of free radicals, while also filtering out longer wavelengths of visible light. Therefore, afamelanotide is photoprotective against visible light photosensitivity and, thus, it is an effective treatment option for disorders such as erythropoietic protoporphyria (EPP), solar urticaria, and polymorphic light eruption (PMLE). (See Introduction Section.) Moreover, McNeil teaches afamelanotide, an α-melanocyte stimulating hormone analogue, has become an emerging therapeutic option for a variety of skin conditions previously refractory to other treatments. Its efficacy has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. Its relatively low risk side effect profile makes it an attractive treatment option and also paves the way for innovative use in other disorders. (See Abstract.) McNeil further teaches Solar urticaria is a chronic photosensitivity disorder characterized by an itch, wheal and flare reaction that occurs within minutes of sunlight exposure. (See Solar Urticaria Section.)
It would have been prima facie obvious to one of ordinary skill in the art at the time the invention was filed to modify the method taught by the U.S patent by including a solar urticaria, intravenous, topical, oral, and percutaneous (reading of transdermal) administration and 50-600 mg/day to give Applicant’s claimed invention. One would have been motivated to do so, because the U.S. patent teaches the compound has melanocortin 1 receptor (MC1R) agonistic activity, because Yamamoto teaches the compound has melanocortin 1 receptor (MC1R) agonistic activity can be administered in the amount of 0.01 to 500 mg/day, where said amount substantially overlap with the amount claimed, because Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease, and also because McNeil teaches other MC1R agonist such afamelanotide has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. One would reasonably expect the method of the compound of the U.S. patent to successfully treat solar urticaria with success.
Claims 1, 5-6, 12-15, and 17-27 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-5 of U.S. Patent No. 11,053,217 B2 in view of Yamamoto et al (9,981,960 B2), Bouix-Peter (US9,353,083 B2) in view of McNeil et al (Skin Therapy Letter, Volume 23 Number 6, December 1, 2018).
The U.S. patent teaches Methyl 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidine-3-carbonyl]-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl} piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid, which is represented by formula (1):
PNG
media_image3.png
770
901
media_image3.png
Greyscale
2. A 1/2 ethane-1,2-disulfonic acid salt of a compound (1′):
PNG
media_image4.png
500
835
media_image4.png
Greyscale
wherein the compound is in crystalline form. (See claim 1.)
The U.S. patent does not teach solar urticaria as the elected photoallergic dermatitis and adverse effect of phototherapy.
Yamamoto teaches a method for treating diseases and/or symptoms in which activation of melanocortin 1 receptor (MC1R) is involved, the method comprising administering to a patient an effective amount of a pyrrolidine compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the diseases and/or symptoms is rheumatoid arthritis, gouty arthritis, osteoarthrosis, inflammatory bowel disease, systemic sclerosis, psoriasis, fibrosis, protoporphyria, systemic lupus erythematosus, melanoma, skin cancer, vitiligo, hair loss, pain, ischemia/reperfusion damage, cerebral inflammatory disease, hepatitis, septicemia/septic shock, nephritis, transplantation, HIV disease exacerbation, vasculitis, uveitis, retinitis pigmentosa, age-related macular degeneration, celiac disease, nephrotic syndrome, or melanoma invasion. (See claims 1 and 25.) Moreover, Yamamoto teaches the compound of the formula (I) includes 1-{2-[(3S,4R)-1-{[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidin-3-yl] carbonyl}-4-(methoxymethyl) pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl} piperidine-4-carboxylic acid. (See claim 18.) This compound is the same as the claimed elected compound. Yamamoto teaches the compound can be administered to a patient (a human or animal) using an appropriate method of administration in accordance with the dosage form (e.g., intravenously, orally, percutaneously, or topically). (See lines 51-57 of column 64.) Percutaneous is the same as transdermal. Furthermore, Yamamoto teaches the compound can be used preferably in about 0.01 to 500 mg/person/day. (See lines 1-11 of column 65.)
Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease. (See claim 4.)
McNeil afamelanotide is composed of a linear peptide of thirteen amino acids, two of which differ from α-MSH. These two different amino acids increase the affinity of afamelanotide to the melanocortin 1 receptor (MC1R), which in turn increase the stability, potency, and half-life of afamelanotide. Afamelanotide, like α-MSH, binds to MC1R in dermal cells and in melanocytes, thereby stimulating melanocyte production of eumelanin as well as melanocyte proliferation. Eumelanin exhibits numerous roles, including photoprotection against ultraviolet (UV) light and scavenging of free radicals, while also filtering out longer wavelengths of visible light. Therefore, afamelanotide is photoprotective against visible light photosensitivity and, thus, it is an effective treatment option for disorders such as erythropoietic protoporphyria (EPP), solar urticaria, and polymorphic light eruption (PMLE). (See Introduction Section.) Moreover, McNeil teaches afamelanotide, an α-melanocyte stimulating hormone analogue, has become an emerging therapeutic option for a variety of skin conditions previously refractory to other treatments. Its efficacy has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. Its relatively low risk side effect profile makes it an attractive treatment option and also paves the way for innovative use in other disorders. (See Abstract.) McNeil further teaches Solar urticaria is a chronic photosensitivity disorder characterized by an itch, wheal and flare reaction that occurs within minutes of sunlight exposure. (See Solar Urticaria Section.)
It would have been prima facie obvious to one of ordinary skill in the art at the time the invention was filed to modify the method taught by the U.S. patent by including a solar urticaria, intravenous, topical, oral, and percutaneous (reading of transdermal) administration and 50-600 mg/day to give Applicant’s claimed invention. One would have been motivated to do so, because because Yamamoto teaches the compound has melanocortin 1 receptor (MC1R) agonistic activity can be administered in the amount of 0.01 to 500 mg/day, where said amount substantially overlap with the amount claimed, because Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease, and also because McNeil teaches other MC1R agonist such afamelanotide has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. One would reasonably expect the method of the compound of the U.S patent to successfully treat solar urticaria excluding protoporphyria and vitiligo).
Acknowledgement is made of the receipt and entry of the amendment to the claims filed on January 30, 2026.
Applicant’s argument
Applicant argues Yamamoto is directed to a pyrrolidine compound having
melanocortin receptor agonist activity. Yamamoto broadly describes that the compounds [I] or their pharmaceutically acceptable salts are useful for treating or preventing various immune diseases, inflammation-related diseases and fibrosis-related diseases of which pathological conditions are expected to be improved through the agonist activity of MCIR. As such, Yamamoto describes a wide range of indications and extremely broad ranges of dosages such as 0.0001 to 1000 mg/person/day, 0.001 to 1000 mg/person/day, and 0.01 to 500 mg/person/day. Bouix-Peter is directed to oxazetidine derivatives and describes two oxazetidine derivatives that show improved toxicity and selectivity to hMC1R. Similarly, the McNeil article is directed to afamelanotide, a-melanocyte stimulating hormone (a-MSH) and describes various theories of its efficacy. As such, neither Bouix-Peter nor the McNeil article disclose or suggest the claimed compound, much less its effective amount for treating photodermatosis. Tsurumoto is cited as disclosing the claimed compound in a crystalline form but as noted in the Office Action, Tsurumoto does not teach or suggest solar urticaria and adverse effect of phototherapy. Thus, Tsurumoto does not disclose or suggest the deficiencies addressed in the preceding discussions on Yamamoto, Bouix-Peter and the McNeil article.
Examiner’s response
In response to applicant's arguments against the references individually, one cannot show nonobviousness by attacking references individually where the rejections are based on combinations of references. See In re Keller, 642 F.2d 413, 208 USPQ 871 (CCPA 1981); In re Merck & Co., 800 F.2d 1091, 231 USPQ 375 (Fed. Cir. 1986). In the present case, Yamamoto teaches the compound has melanocortin 1 receptor (MC1R) agonistic activity can be administered in the amount of 0.01 to 500 mg/day, where said amount substantially overlap with the amount claimed. Bouix-Peter teaches a method of treating a disorder and/or disease and/or dysfunction, the method comprising administering a compound of formula (I) below:
PNG
media_image2.png
513
829
media_image2.png
Greyscale
, or an individual subject in need thereof to treat a disease and/or disorder and/or dysfunction includes solar urticaria among other disease. McNeil teaches other MC1R agonist such afamelanotide has been demonstrated in several dermatologic conditions, including erythropoietic protoporphyria (EPP), solar urticaria, polymorphic light eruption (PMLE), vitiligo, acne, and Hailey-Hailey disease. One would reasonably expect the method of the compound of Yamamoto to successfully treat solar urticaria excluding protoporphyria.
Applicant’s argument
Applicant argues Examples 2, 3, 4, 5, 6, and 7 support that the claimed compound or its pharmaceutically acceptable salt or cocrystal treats patients with porphyria when administered in the dosage of 50 to 600 mg/day. Therefore, it is respectfully submitted that the subject matter recited in Claim 1 is believed to be clearly distinguishable from Yamamoto, Bouix-Peter, the McNeil article, and Tsurumoto and their teachings even combined would not render the porphyria treatment method of Claim 1 obvious. Therefore, it is respectfully submitted that the subject matter recited in amended Claim 1 is believed to be clearly distinguishable from Yamamoto, Bouix-Peter, the McNeil article, and Tsurumoto, and their teachings even combined would not render the treatment method of Claim 1 obvious.
Examiner’s response
In response, Applicant’s argument is not persuasive. The Examiner does not dispute that fact that Examples 2-7 demonstrate that exhibited agonist activities on human and mouse MC1R in comparisons with a-MSH and NDP-a-MSH, activates MC1R at a low concentration, induced melanin production in a concentration-dependent manner, results in newly grown significantly blackened body hair after shaving, exhibits a significant increase in expression with respect to TYRP1 and PMEL at the dosages of 100 mg, 300mg and 600 mg, exhibits the maximum increase in melanin density of the skin achieved on day 15 at the dosages of 150 mg and 300 mg and kept until day 29, and exhibits lowering of the skin wrinkle scopes and increased amount of type I collagen in the skin. However, the Examiner contends 100 mg, 300 mg, and 600 mg are not the sole effective amount recited in the claim. Additionally, hair color and skin wrinkles, and porphyria are not recited in the claim. As such, the asserted unexpected blackened body hair after shaving, significant increase in expression TYRP1 and PMEL, and lowering of the skin wrinkle scopes and increased amount of type I collagen in the skin appear to be intended outcome of the method step. The fact that Yamamoto teaches the compound has melanocortin 1 receptor (MC1R) agonistic activity which is the same compound claimed can be administered in amount of 0.01 to 500 mg/day that overlaps with the claimed amount and the fact that the claimed method step is obvious over the teaching of the combined references, one can reasonably expect the overlapping amount of 0.01 to 500 mg/day of the same compound taught to achieve the same intended outcome.
Applicant’s argument
Applicant argues that Claim 1 is believed to be allowable. Furthermore, since Claims 4-7 and 12-27 depend directly or indirectly from Claim 1, substantially the same arguments set forth above also apply to these dependent claims. Hence, claims 4-7 and 12-27 are believed to be allowable as well.
Examiner’s response
In response, Applicant’s argument is not persuasive because claim 1 is not allowable. Therefore, since claims 4-7 and 12-27 depend directly or indirectly from Claim 1, substantially the same response set forth above also apply to these dependent claims.
Conclusion
Claims 1, 5-6, 12-15, and 17-27 are not allowed.
THIS ACTION IS MADE FINAL. Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to JEAN P CORNET whose telephone number is (571)270-7669. The examiner can normally be reached Monday-Thursday from 7.00am-5.30pm.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Amy L Clark can be reached at 571-272-1310. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/JEAN P CORNET/ Primary Examiner, Art Unit 1628